1. Signaling Pathways
  2. Cytoskeleton
  3. Integrin

Integrin

Integrins, a family of heterodimeric adhesion receptors for diverse extracellular matrices, have consistently been implicated as crucial drivers of ovarian cancer development and progression. A number of the RGD-based members of the integrin family, including α5β1, and αvβ3 or αvβ5 integrins, are markedly elevated in aggressive ovarian tumors. These adhesion receptors appear to promote cell adhesion, survival, motility and invasion during ovarian tumor growth or metastatic progression. Importantly, the functions of these integrins are strongly dependent on the activation of focal adhesion kinase (FAK) and its downstream signaling, including the PI3K/Akt- and Ras/MAPK-dependent pathways.

Integrins are transmembrane proteins and are major receptors for cell-extracellular matrix (ECM) and cell-cell adhesion. Modulation of these molecules, particularly αv integrin family, has exhibited profound effects on fibrosis in multiple organ and disease state. Based on the several studies, the integrins αvβ3, αvβ5, αvβ6, and αvβ8 have been known to modulate the fibrotic process via activation of latent transforming growth factor (TGF)-β in pre-clinical models of fibrosis.

Each integrin is typically formed by the non-covalent pairing of one α subunit, of which, 18 types are known to exist, and one β subunit, of which 8 types are known to exist. Together, 24 distinct heterodimers have been identified to date. The αv subunit can form heterodimers with the β1, β3, β5, β6 or β8 subunits and β1 can associate with many different α subunits from α1 to α11, and αv, indicating that not all theoretically possible α and subunit pairs form. Interestingly, the activation of TGF-β appears to be a common function of multiple αv integrins.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-70073
    Zaurategrast
    Inhibitor 98.07%
    Zaurategrast (CT7758) is a potent and oral-effective α4-integrin inhibitor.
    Zaurategrast
  • HY-P990643
    OS-2966
    Inhibitor 99.62%
    OS-2966 is a humanized antibody expressed in CHO cells, targeting Integrin b1/ITGB1/CD29. OS-2966 carries a huIgG1 type heavy chain and a huκ type light chain, with a predicted molecular weight (MW) of 145.5 kDa. The isotype control for OS-2966 can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
    OS-2966
  • HY-P1654
    A20FMDV2
    Inhibitor 98.03%
    A20FMDV2 is a selective αvβ6 integrin inhibitor (IC50: 3 nM), with an activity 1,000-fold more selective for αvβ6 than for other RGD-directed integrins (αvβ3, αvβ5, and α5β1). A20FMDV2 can be derived from the foot-and-mouth disease virus. A20FMDV2 can be radiolabeled for the PET imaging of αvβ6 integrin-positive tumors.
    A20FMDV2
  • HY-10596
    BMS-688521
    Inhibitor 98.62%
    BMS-688521 is a highly potent, orally active inhibitor of the LFA-1/ICAM interaction, with an IC50 of 2.5 nM in the adhesion assay and an IC50 of 60 nM in the MLR assay. BMS-688521 is efficacious in a mouse allergic eosinophilic lung inflammation model.
    BMS-688521
  • HY-164768
    LT25
    Agonist 98.73%
    LT25 (compound 17) is a agonist of α5β1 integrin with EC50 value of 9.9 nM.
    LT25
  • HY-P1408
    Obtustatin
    Inhibitor 99.69%
    Obtustatin is a non-RGD disintegrin of 41 residues. Obtustatin can be isolated from Vipera lebetina obtusa venom. Obtustatin is a potent and selective inhibitor of the adhesion of integrin α1β1 to collagen IV. Obtustatin inhibits angiogenesis, and can be used for research of cancer.
    Obtustatin
  • HY-48959
    α7β1 integrin modulator-1
    Modulator 98.02%
    α7β1 integrin modulator-1 is a potent α7β1 integrin modulator. α7β1 integrin modulator-1 has the potential for the research of muscular dystrophy.
    α7β1 integrin modulator-1
  • HY-P0290A
    GRGDSP TFA
    Inhibitor ≥98.0%
    GRGDSP (TFA) is an integrin inhibitor.
    GRGDSP TFA
  • HY-P2452
    Vitronectin (367-378)
    99.78%
    Vitronectin (367-378) is a peptide corresponding to residues 367-378 of Vitronectin. Vitronectin is a multifunctional glycoprotein known in several human tumors for its adhesive role in processes such as cell growth, angiogenesis and metastasis.
    Vitronectin (367-378)
  • HY-P2267
    LDV
    Inhibitor 99.27%
    LDV is a non-fluorescent analog of LDV-FITC. LDV is a α4β1 integrin (VLA-4) ligand, and binds α4β1 integrin in leukemia cells.
    LDV
  • HY-148385
    Ganglioside GM2
    98.0%
    Ganglioside GM2 is a human tumor antigen predominantly found in human tumor cells and fetal brain tissue. As a sialylated glycosphingolipid, Ganglioside GM2 is involved in processes such as cell signaling, adhesion, and motility. Ganglioside GM2 abnormal expression and accumulation are associated with tumors and neurodegenerative disorders. Ganglioside GM2 promotes tumor cell migration and invasion by directly binding to the integrin β1 receptor, activating the FAK/Src/Erk-MAPK signaling pathway, and inducing actin cytoskeleton remodeling.
    Ganglioside GM2
  • HY-12308
    TCS 2314
    Antagonist ≥99.0%
    TCS 2314 (compound 3) is orally active and selective very late antigen-4 (VLA-4, α4β1, CD49d/CD29) antagonist with an IC50 of 4.4 nM.
    TCS 2314
  • HY-P99891
    Rovelizumab
    Inhibitor
    Rovelizumab is a humanized monoclonal leukointegrin antibody. Rovelizumab is a monoclonal antibody directed against the CD11/CD18 cell adhesion proteins. Rovelizumab can be used for research of multiple sclerosis (MS), hemorrhagic shock, myocardial infarction (MI) and stroke.
    Rovelizumab
  • HY-P5287A
    cRGDfK-thioacetyl ester TFA
    Chemical 99.02%
    cRGDfK-thioacetyl ester TFA is a bioactive polypeptide molecule. cRGDfK peptide has a selective affinity for integrins. cRGDfK peptide can modify NIR fluorescent probes for cancer targeting imaging.
    cRGDfK-thioacetyl ester TFA
  • HY-P3732
    RGD-4C
    99.82%
    RGD-4C is a arginine-glycine-aspartic acid peptide (ACDCRGDCFC) with integrin binding activity. The Arg-Gly-Asp (RGD) sequence serves as the primary integrin recognition site in extracellular matrix proteins, and peptides containing this sequence can mimic the recognition specificity of the matrix proteins. RGD-4C is a αv-integrin ligand, can conjugate with bioactive molecule to exert antitumor effects in animal models.
    RGD-4C
  • HY-P3522A
    REDV TFA
    99.81%
    REDV TFA is the minimal active sequence within the CS5 site of the alternatively spliced type III connecting segment (IIICS) region of fibronectin. REDV TFA can mediate adhesion to the IIICS region of plasma fibronectin by binding the integrin alpha 4 beta 1(α4β1). REDV TFA can be used for the research of cell adhesion.
    REDV TFA
  • HY-119350B
    Zalunfiban dihydrochloride
    99.07%
    Zalunfiban (RUC-4) dihydrochloride is a potent, selective platelet αIIbβ3 antagonist (IC50=45 nM). Zalunfiban dihydrochloride can be used for the research of myocardial infarction (MI).
    Zalunfiban dihydrochloride
  • HY-19306
    SB-267268
    Antagonist 99.85%
    SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression.
    SB-267268
  • HY-14277A
    Levocabastine hydrochloride
    Antagonist 99.3%
    Levocabastine (R 50547) hydrochloride is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC).
    Levocabastine hydrochloride
  • HY-P6022
    G4RGDSP, integrin-binding peptide
    99.61%
    G4RGDSP, Integrin-binding peptide is a cell integrin-binding peptide that targets integrin receptors. G4RGDSP, integrin-binding peptide is coupled to alginate to increase the viability of cells in the scaffold. G4RGDSP, integrin-binding peptide can be used as an extrudable carrier for chondrocyte delivery for the study of 3D printing technology
    G4RGDSP, integrin-binding peptide
Cat. No. Product Name / Synonyms Species Source
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